C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 7/08 (2006.01) A61K 31/787 (2006.01) A61K 38/00 (2006.01) A61P 31/04 (2006.01) C07K 7/02 (2006.01) C07K 7/06 (2006.01)
Patent
CA 2671358
This invention encompasses synthetic antimicrobial peptide analogs having certain un-natural amino acids, including the un-natural amino acids hydrophobic tetrahydroisoquinolinecarboxylic acid (Tic) and octahydroindolecarboxylic acid (Oic), incorporated into the polypeptide backbone. These antimicrobial peptides (AMPs) are useful to treat infection in humans and other mammals of such bacteria as Gram positive bacteria, Gram negative bacteria and Mycobacterium. Many of the AMPs also exhibit the property of reduced hemolytic activity. The invention also entails 3D-QSAR models and mathematical equations that calculate the biological activity of any peptide sequence against Staphylococcus aureus or Mycobacterium ranae.
Analogues peptidiques antimicrobiens synthétiques comportant certains acides aminés non naturels, y compris les acides aminés suivants: acide tétrahydroisoquinolinecarboxylique (Tic) et octahydroindolecarboxylique (Oic) hydrophobe. Ces acides sont incorporés dans le squelette polypeptidique. Les peptides antimicrobiens (AMP) sont utiles pour traiter l'infection chez l'être humain et d'autres mammifères, par des bactéries du type Gram positif, Gram négatif et Mycobacterium. Par ailleurs, de nombreux AMP offrent une propriété de réduction d'activité hémolytique. On décrit enfin des modèles 3D-QSAR et des équations mathématiques permettant d'évaluer l'activité biologique d'une séquence peptidique quelconque contre Staphylococcus aureus ou Mycobacterium ranae.
Bhonsle Jayendra
Hicks Rickey P.
Venugopal Divakaramenon
Gowling Lafleur Henderson Llp
On Behalf Of Walter Reed Army Institute Of Research The United States Of America As Represented By The Secretary Of
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